Choline chloride
Based on 6 publication(s) in Google Scholar
Choline chloride is an orally active methylxanthine derivative. Choline chloride exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline chloride relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. Choline chloride modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline chloride is used in studies of bronchospasm, nocturnal asthma, and chronic asthma.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 67-48-1
- Formula: C5H14ClNO
- Molecular Weight:139.62
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Storage:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Choline chloride
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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RT-PCR
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In Vivo Efficacy Study
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RT-PCR
All Histamine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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Human Endogenous Metabolite |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
17 μM
Compound: 6209
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Substrate uptake and inhibition of the High Affinity Choline Transporter 1 (CHT1, SLC5A7) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC5A7 cells
Substrate uptake and inhibition of the High Affinity Choline Transporter 1 (CHT1, SLC5A7) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC5A7 cells
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10.5281/zenodo.7361355 |
| HEK293 | EC50 |
17 μM
Compound: 6209
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Substrate uptake and inhibition of the High Affinity Choline Transporter 1 (CHT1, SLC5A7) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC5A7 cells (PubChem AID: 1794811)
Substrate uptake and inhibition of the High Affinity Choline Transporter 1 (CHT1, SLC5A7) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC5A7 cells (PubChem AID: 1794811)
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10.5281/zenodo.7361355 |
In Vitro
Choline chloride (Choline theophyllinate) (100 μg/mL; 15 min) causes concentration-dependent relaxation of isolated guinea-pig tracheal bronchial muscle and is used as a reference bronchodilator in this preparation[1].
Choline chloride (Choline theophyllinate) exhibits very weak antihistamine and anti-acetylcholine activity on isolated guinea-pig ileum, with initial potentiation of agonist responses during exposure and weak reduction after washout[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Choline chloride (Choline theophyllinate) (50-200 mg/kg; p.o.; single dose) protects guinea-pigs against acetylcholine-induced bronchospasm with maximum effect at 1 hr and measurable activity persisting for at least 6 hr at higher doses[1].
Choline chloride (Choline theophyllinate) (10 mg/kg; i.v.) produces a pronounced increase in urine flow in anaesthetized rabbits[1].
Choline chloride (Choline theophyllinate) (74-337 mg/kg; i.v.; p.o.) has an acute oral LD50 of 337 mg/kg in albino mice and an intravenous LD50 of 74 mg/kg, with an oral-to-intravenous ratio of 4.5 indicating good gastrointestinal absorption[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea-pigs (8 per treatment group)[1]
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Dosage:50 mg/kg (acetylcholine 30% protection, histamine 19% protection); 100 mg/kg (acetylcholine 61% protection, histamine 69% protection)
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Administration:i.p.; single dose 20 min before aerosol challenge
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Result:Provided 30% mean percentage protection against 4% acetylcholine-induced bronchospasm at 50 mg/kg.
Provided 19% mean percentage protection against 2% histamine-induced bronchospasm at 50 mg/kg.
Provided 61% mean percentage protection against 4% acetylcholine-induced bronchospasm at 100 mg/kg.
Provided 69% mean percentage protection against 2% histamine-induced bronchospasm at 100 mg/kg.
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Animal Model:Guinea-pigs (32 total, 4 per time point per compound)[1]
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Dosage:50 mg/kg; 200 mg/kg (activity persists at 6 hr)
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Administration:p.o.; single dose by stomach tube
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Result:Reached maximum protective effect against acetylcholine-induced bronchospasm at 1 hr after oral administration.
Retained some protective effect at 6 hr after dosing at the 200 mg/kg dose.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 67-48-1
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Appearance Solid
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Molecular Weight 139.62
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Formula C5H14ClNO
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Color White to off-white
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SMILES
OCC[N+](C)(C)C.[Cl-]
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
DHRS2 inhibits cell growth and metastasis in ovarian cancer by downregulation of CHKα to disrupt choline metabolism. [Abstract]2022 Oct 3;13(10):845. PMID: 36192391 -
Phytomedicine
Motherwort synergized with oxytocin for postpartum hemorrhage prevention: Integrated clinical efficacy and mechanism exploration. [Abstract]2025 Sep:145:156951. PMID: 40527062 -
J Hazard Mater
EHDPP impairs intestinal microbiota homeostasis and induces placental injury through choline mediated gut-placenta axis. [Abstract]2025 Jun 5:489:137573. PMID: 40007358
Choline chloride purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline (30 μM, 24 h) demonstrated no cytotoxic effects but partially mitigated the inhibition of cell viability induced by EHDPP in HTR-8/SVneo and JEG-3 cells.
Choline chloride purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline (30 μM, 24 h) reversed EHDPP-induced cell migration inhibition in HTR-8/SVneo cells.
Choline chloride purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline (30 μM, 24 h) reversed the EHDPP-induced decrease of mRNA levels of TNF-α, IL-6, and IL-1β in HTR-8/SVneo cells.
Choline chloride purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline supplementation (25 mM choline-containing water for 31.5 days) significantly increased uterine size, fetal weight, placental weight, and placental diameter that were reduced by EHDPP exposure.
Choline chloride purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline supplementation (25 mM choline-containing water for 31.5 days) alleviated the decrease in mRNA expression of the proliferation marker Ki67 and the vascular differentiation marker CD31 induced by EHDPP.
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Antioxidants (Basel)
Role of Mitochondrial Reactive Oxygen Species-Mediated Chaperone-Mediated Autophagy and Lipophagy in Baicalin and N-Acetylcysteine Mitigation of Cadmium-Induced Lipid Accumulation in Liver. [Abstract]2024 Jan 17;13(1):115. PMID: 38247538 -
Solvent & Solubility
In Vitro:
DMSO : ≥ 140 mg/mL (1002.72 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (716.23 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.5 mg/mL (25.07 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.5 mg/mL (25.07 mM); Clear solution
This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 130 mg/mL (931.10 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 7.1623 mL | 35.8115 mL | 71.6230 mL | 179.0574 mL |
| 5 mM | 1.4325 mL | 7.1623 mL | 14.3246 mL | 35.8115 mL | |
| 10 mM | 0.7162 mL | 3.5811 mL | 7.1623 mL | 17.9057 mL | |
| 15 mM | 0.4775 mL | 2.3874 mL | 4.7749 mL | 11.9372 mL | |
| 20 mM | 0.3581 mL | 1.7906 mL | 3.5811 mL | 8.9529 mL | |
| 25 mM | 0.2865 mL | 1.4325 mL | 2.8649 mL | 7.1623 mL | |
| 30 mM | 0.2387 mL | 1.1937 mL | 2.3874 mL | 5.9686 mL | |
| 40 mM | 0.1791 mL | 0.8953 mL | 1.7906 mL | 4.4764 mL | |
| 50 mM | 0.1432 mL | 0.7162 mL | 1.4325 mL | 3.5811 mL | |
| 60 mM | 0.1194 mL | 0.5969 mL | 1.1937 mL | 2.9843 mL | |
| 80 mM | 0.0895 mL | 0.4476 mL | 0.8953 mL | 2.2382 mL | |
| 100 mM | 0.0716 mL | 0.3581 mL | 0.7162 mL | 1.7906 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Choline chloride Related Classifications
HY-B1337 Related Classifications
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